Design, synthesis, and biological evaluation of novel 1, 2, 4-triazole derivatives as antifungal agent

被引:11
作者
Chai, Xiaoyun [1 ]
Yu, Shichong [1 ]
Jiang, Yongwei [1 ]
Zou, Yan [1 ]
Wu, Qiuye [1 ]
Zhang, Dazhi [1 ]
Jiang, Yuanying [2 ]
Cao, Yongbing [2 ]
Sun, Qingyan [1 ]
机构
[1] Second Mil Med Univ, Sch Pharm, Dept Organ Chem, Shanghai 200433, Peoples R China
[2] Second Mil Med Univ, Sch Pharm, Drug Res Ctr, Shanghai 200433, Peoples R China
基金
中国国家自然科学基金;
关键词
Triazole; Synthesis; Antifungal activity; CACYP51; Molecular docking; TRIAZOLE DERIVATIVES; ASPERGILLOSIS;
D O I
10.1007/s12272-012-1105-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of novel 1, 2, 4-triazole derivatives (9a-p) have been designed and synthesized as the potential antifungal agents. All compounds were characterized by H-1-NMR, C-13-NMR, and LCMS. Their antifungal activities against seven human pathogenic fungi were evaluated in vitro by measuring the minimal inhibitory concentrations. Most of the tested compounds were found to be more potent against Candida albicans than the control drug fluconazole.
引用
收藏
页码:1895 / 1901
页数:7
相关论文
共 16 条
  • [1] [Anonymous], 2002, CLSI document M27-A2, V2nd
  • [2] [Anonymous], 2010, EUR J MED CHEM, DOI DOI 10.1016/j.ejmech.2010.07.002
  • [3] New azoles with antifungal activity: Design, synthesis, and molecular docking
    Chai, Xiaoyun
    Zhang, Jun
    Cao, Yongbing
    Zou, Yan
    Wu, Qiuye
    Zhang, Dazhi
    Jiang, Yuanying
    Sun, Qingyan
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (02) : 686 - 689
  • [4] Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14α-demethylase
    Chai, Xiaoyun
    Zhang, Jun
    Hu, Honggang
    Yu, Shichong
    Sun, Qingyan
    Dan, Zhigang
    Jiang, Yuanying
    Wu, Qiuye
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (05) : 1913 - 1920
  • [5] ANALOGS OF NUCLEOSIDES .43. PREPARATION OF RIBOSYL DERIVATIVES OF 1,2,4-TRIAZOL-3(2H)-ONE AND 5-METHYL-1,2,4-TRIAZOL-3(2H)-ONE
    HREBABECKY, H
    BERANEK, J
    [J]. COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS, 1985, 50 (03) : 779 - 788
  • [6] Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents
    Jiang, Yongwei
    Zhang, Jun
    Cao, Yongbing
    Chai, Xiaoyun
    Zou, Yan
    Wu, Qiuye
    Zhang, Dazhi
    Jiang, Yuanying
    Sun, Qingyan
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (15) : 4471 - 4475
  • [7] Design, synthesis and antifungal evaluation of 1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-1,2,4-triazol-5(4H)-one
    Jiang, Yongwei
    Cao, Yongbin
    Zhang, Jun
    Zou, Yan
    Chai, Xiaoyun
    Hu, Honggang
    Zhao, Qingjie
    Wu, Qiuye
    Zhang, Dazhi
    Jiang, Yuanying
    Sun, Qingyan
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2011, 46 (07) : 3135 - 3141
  • [8] Krishnamurthy N., 1998, US Patent, Patent No. 5728834
  • [9] History of the development of azole derivatives
    Maertens, JA
    [J]. CLINICAL MICROBIOLOGY AND INFECTION, 2004, 10 : 1 - 10
  • [10] EPIDEMIOLOGY AND ANTIFUNGAL RESISTANCE IN INVASIVE ASPERGILLOSIS ACCORDING TO PRIMARY DISEASE - REVIEW OF THE LITERATURE
    Mayr, A.
    Lass-Floerl, C.
    [J]. EUROPEAN JOURNAL OF MEDICAL RESEARCH, 2011, 16 (04) : 153 - 157